Amlodipine | Norvasc, Aforbes | Cav1.x inhibitor | Hypertension, vasospastic angina, angina pectoris | Small molecule | 1992 | Pfizer |
Ajmaline | | Nav1.5 inhibitor | Arrhythmia | Small Molecule | | |
Alosetron | Lotronex | 5HT3A antagonist | Irritable bowel syndrome with diarrhea | Small molecule | 2002 FDA | |
Alprazolam | Xanax | GABA-A positive modulator | Anxiety | Small molecule | 1981 FDA | Upjohn |
Amantadine | Symadine, Osmolex | GluN inhibitor | Parkinson's disease | Small molecule | | |
Amifampridine | Firdapse | Kv blocker | Lambert-Eaton myasthenic syndrome | Small molecule | 2009 | BioMarin |
Amiloride | Midamor | ENaC inhibitor | Hypertensive disorder, edema, hypokalemia | Small molecule | 1981 | |
Amiodarone | Cordarone | Kv11.1 blocker | Ventricular fibrillation, life-threatening ventricular tachycardia | Small molecule | 1961 | |
Atracurium | | Chrn abd antagonist | General anaesthesia, muscle relaxation | Small Molecule | 1983 FDA | |
Azelnidipine | CalBlock | Cav1.x blocker | Hypertension | Small Molecule | | Daiichi-Sankyo |
Benzocaine | Anacaine, Dermoplast | Nav blocker | Local anesthesia | Small Molecule | | |
Bioallethrin | | Sodium channel (Pediculus humanus) modulator | Lice and scabies infestation | Small Molecule | | |
Brexanolone | Zulresso | GABA-A positive modulator | Postpartum depression | Small Molecule | 2019 | Sage Therapeutics |
Bupivacaine | Marcaine | Nav inhibitor | Local anesthesia | Small molecule | 1972 FDA | Hospira |
Butalbital | Sandoptal | GABA-A potentiator | Tension-type headache | Small Molecule | 1976 | Actavis Labs |
Capsaicin | Zostrix, Qutenza | TRPV1 activator | Neuralgia, postherpetic neuralgia, backache, arthritic pain | Small molecule | 2009 FDA | Acorda Therapeutics |
Carbamazepine | Actebral, Tegretol | Nav1.5 blocker | Epilepsy, Lennox-Gastaut syndrome, bipolar disorder | Small molecule | 1968 | Novartis |
Carbutamide | Glucidoral | Kir6.2 inhibitor | Diabetes mellitus type 2 | Small molecule | 1956 | Servier |
Chlordiazepoxide | Risolid | GABAA positive modulator | Anxiety, alcohol withdrawal syndrome | Small molecule | 1960 FDA | Valeant |
Chloroprocaine | Nesacaine | Nav1.8 inhibitor | Local anesthesia | Small Molecule | | |
Chlorpropamide | | Kir6.2 inhibitor | Diabetes mellitus type 2 | Small molecule | 1958 | Pfizer |
Chlorzoxazone | Parafon, Paraflex | KCa activator | Spasticity, muscle spasm with pain | Small molecule | 1958 | Janssen |
Cilnidipine | Atelec, Cilogard | Cav1.x blocker, Cav2.2 blocker | Hypertension | Small Molecule | 1995 | Fuji Viscera, Ajinomoto |
Cinchocaine | Dibucaine, Nupercainal | Nav blocker | Local anesthesia | Small Molecule | | |
Cinnarizine | Stugeron, Cinazyn | Cav inhibitor | Vertigo, motion sickness, nausea | Small molecule | 1955 | Jansen Pharmaceutica |
Cisatracurium | Nimbex | Chrn a1b1d inhibitor | General anaesthesia, muscle relaxation | Small molecule | 1995 FDA | |
Clevidipine | Cleviprex | Cav1.x blocker | Hypertension | Small molecule | 2008 | The Medicines Company |
Clobazam | Frisium, Urbanol, Onfi, Tapclob | GABAA partial agonist | Epilepsy, anxiety | Small molecule | 2011 | Lundbeck |
Clonazepam | Clonapam, Rivotril | GABAA positive modulator | Myoclonic, atonic and absence seizures; Lennox-Gastaut syndrome | Small molecule | 1975 | Roche |
Clorazepate | Tranxene | GABAA positive modulator | Anxiety, alcohol withdrawal syndrome, partial epilepsy | Small molecule | 1972 | |
Clotiazepam | Clozan | GABA-A potentiator | Anxiety disorders | Small Molecule | | |
Crofelemer | Mytesi, Fulyzaq | CFTR inhibitor, ANO1 inhibitor | Non-infectious diarrhea | Small Molecule | 2012 | Salix Pharmaceuticals |
Cyclandelate | Cyclospasmol | Cav alpha-2/delta-1 modulator | Arteriosclerosis, Raynaud's disease | Small Molecule | | |
Dalfampridine | Ampyra, Fampyra | Kv blocker | Multiple sclerosis | Small molecule | 2010 | Acorda Therapeutics |
Dantrolene | Dantrium | RyR1 inhibitor | Spasticity, malignant hyperthermia | Small molecule | 1974 | Par Pharmaceutical |
Desflurane | Suprane | GABA-A agonist, GluA1 inhibitor, GLYRA1 agonist | General anestesia | Small Molecule | 1992 | Baxter |
Dextromethorphan | | GluN3A antagonist | Cough, rhinitis, sneezing | Small Molecule | 1957 | ANI Pharmaceuticals |
Diazepam | Valium, Diastat | GABA-A potentiator | Anxiety, alcohol withdrawal syndrome, spasticity, epilepsy | Small molecule | 1963 FDA | Roche |
Diazoxide | Proglycem | Kir6.2 activator | Hypertensive emergencies, hyperinsulinism | Small molecule | 1973 | |
Diltiazem | Cardizem, Tiazac | Cav1.x inhibitor | Hypertension, angina pectoris | Small molecule | 1982 | |
Disopyramide | Norpace, Ritmodan, Dicorantil | Nav1.5 inhibitor | Ventricular arrhythmia | Small molecule | 1977 | G.D. Searle LLC |
Dofetilide | Tikosyn | Kir2.2, Kv10.1, Kv11.1 inhibitor | Atrial fibrillation, atrial flutter | Small molecule | 1999 | Pfizer |
Dronedarone | Multaq | Multichannel blocker | Atrial fibrillation | Small molecule | 2009 FDA | Sanofi-Aventis |
Efonidipine | Landel | Cav1.x inhibitor, Cav3.x inhibitor | Hypertension | Small molecule | 1995 | |
Enflurane | Ethrane, Alyrane | GABA-A agonist, GluA1 inhibitor, GLYRA1 agonist | General anestesia | Small Molecule | 1972 | Baxter |
Eslicarbazepine | Aptiom, Zebinix, Exalief | Nav inhibitor | Partial seizures | Small molecule | 2009 EMA 2013 FDA | Bial |
Estazolam | Prosom, Eurodin, Nuctalon | GABAA potentiator | Severe Insomnia | Small molecule | 1990 | Abbott |
Eszopiclone | Lunesta | GABA-A potentiator | Insomnia | Small molecule | 2004 | Sunovion |
Ethosuximide | Zarontin | Cav3.1 inhibitor | Absence seizures | Small molecule | 1960 | Parke Davis |
Etidocaine | Duranest | Nav inhibitor | Local anesthesia | Small molecule | 1976 FDA | |
Felbamate | Felbatol | GluN antagonist | Epilepsy, Lennox-Gastaut syndrome | Small molecule | 1993 FDA | |
Felodipine | Plendil | Cav1.x blocker, Cav3.x blocker | Hypertension, Angina pectoris prophylaxis | Small molecule | 1991 | AstraZeneca |
Flecainide | Tambocor | Nav1.4 and Nav1.5 blocker | Atrial fibrillation, atrial flutter, life-threatening ventricular tachycardia | Small molecule | 1985 | |
Flumazenil | Anexate, Romazicon | GABA-A antagonist | Benzodiazepine induced sedation or toxicity | Small molecule | 1991 FDA | Hoffman La Roche |
Flunarizine | Sibelium | Cav3.x inhibitor | Migraine, epilepsy, vertigo | Small molecule | 1968 | Jansen Pharmaceutica |
Flunitrazepam | Hypnodorm | GABA-A potentiator | Severe insomnia, anxiety | Small Molecule | 1976 | |
Flupirtine | Katadolon | Kv7.2-Kv7.5 activator | Acute and chronic pain | Small molecule | 1984 | Asta-Medica |
Flurazepam | Dalmadorm, Dalmane | GABAA activator | Insomnia | Small molecule | 1970 | |
Fluspirilene | Redeptin, Imap | Cav inhibitor | Schizophrenia | Small molecule | 1963 | Jansen Pharmaceutica |
Fosphenytoin | Cerebyx | Nav1.5 blocker | Epilepsy | Small molecule | 1996 | Parke-Davis |
Funapide | TV-45070, XEN402 | Nav1.7 and Nav1.8 blocker | Chronic pain | Small Molecule | | Xenon Pharmaceuticals |
Gabapentin | Neurontin | Cav alpha-2/delta inhibitor, GluN inhibitor | Postherpetic neuralgia, partial seizures | Small molecule | 1993 | Pfizer |
Glibenclamide | Diabeta, Glyburide | Kir6.2 inhibitor | Diabetes mellitus type 2 | Small molecule | 1984 | Sanofi Aventis |
Glibornuride | Glutril | Kir6.2 inhibitor | Diabetes mellitus type 2 | Small molecule | 1969/ | |
Gliclazide | Diamicron | Kir6.2 inhibitor | Diabetes mellitus type 2 | Small molecule | 1972 | |
Glimepiride | Amaryl | Kir6.2 inhibitor | Diabetes mellitus type 2 | Small molecule | 1995 | Sanofi Aventis |
Glipizide | Glucotrol | Kir6.2 inhibitor | Diabetes mellitus type 2 | Small molecule | 1984 | Pfizer |
Gliquidone | Glurenorm | Kir6.2 blocker | Diabetes mellitus type 2 | Small Molecule | | |
Glisoxepide | | Kir6.x inhibitor | Diabetes mellitus type 2 | Small molecule | | |
Glyclopyramide | Deamelin | Kir6.x inhibitor | Diabetes mellitus type 2 | Small molecule | 1965 | |
Glymidine | Glycanol | Kir inhibitor | Diabetes mellitus type 2 | Small Molecule | | |
Granisetron | Kytril | 5HT3A antagonist | Therapy-induced nausea and vomiting | Small molecule | 1993 FDA | |
Halothane | | GABA-A agonist, GluA1 inhibitor, GLYRA1 agonist | General anesthesia | Small Molecule | 1958 FDA | |
Hexylcaine | Cyclaine | Nav blocker | Local anesthesia | Small Molecule | | Merck |
Ibutilide | Corvert | Kv11.1 blocker | Atrial fibrillation, atrial flutter | Small Molecule | 1995 | |
Isoflurane | Isorane, Aerrane | GABA-A agonist, GluA1 inhibitor, GLYRA1 agonist | General anestesia | Small Molecule | 1979 | Baxter |
Isradipine | DynaCirc, Prescal, Clivoten, Esradin, Lomir | Cav1.x blocker | Hypertension | Small molecule | 1989 | Sandoz (now division of Novartis) |
Ivabradine | Corlanor, Corlentor | HCN inhibitor | Chronic heart failure, angina pectoris | Small molecule | 2005 EMA 2015 FDA | Servier, Amgen |
Ivacaftor | Kalydeco | CFTR potentiator | Cystic fibrosis | Small molecule | 2012 | Vertex Pharmaceuticals |
Ketamine | Ketalar | GluN antagonist | General and local anaesthesia | Small molecule | 1970 FDA | |
Ketazolam | Loftran, Anseren | GABA-A potentiator | Anxiety | Small Molecule | | |
Lacidipine | Lacipil, Motens | Cav1.x blocker | Hypertension | Small Molecule | | |
Lacosamide | Vimpat | Nav inhibitor | Partial epilepsy | Small molecule | 2008 FDA 2008 EMA | UCB |
Lamotrigine | Lamictal | Nav inhibitor | Tonic-clonic seizures, epilepsy, Lennox-Gastaut syndrome | Small molecule | 1994 | GSK |
Leconotide | | Cav2.2 blocker | Pain | Peptide | | |
Lercanidipine | Zanidip | Cav1.x inhibitor | Hypertension | Small molecule | 1997 | |
Levamlodipine | Asomex, Espin | Cav1.x blocker | Hypertension, angina | Small Molecule | | |
Levobupivacaine | Chirocaine | Nav inhibitor | Local anesthesia | Small molecule | 1999 FDA | Purdue pharma |
Levomenthol | Menthol | TRPM8 agonist | Minor irritation, pain, sore mouth, sore throat, itching, local anesthesia | Small Molecule | | |
Lidocaine | Xylocaine | Nav blocker | Local anaesthesia, neuralgia, itching, pediculosis, ventricular arrhythmia | Small molecule | 1948 | Fresenius Kabi |
Lorazepam | Ativan | GABAA activator | Anxiety, Myoclonic seizure, Atonic seizure, Status epilepticus | Small molecule | 1977 FDA | Wyeth Pharmaceuticals |
Lormetazepam | | GABA-A potentiator | Short-term insomnia | Small Molecule | | |
Lubiprostone | Amitiza | CLC-2 activator | Chronic idiopathic constipation | Small Molecule | 2006 | Sucampo Pharmaceuticals |
Lumacaftor | Orkambi (a combination of ivacaftor and lumacaftor) | CFTR modulator | Cystic fibrosis | Small molecule | 2015 | Vertex Pharmaceuticals |
Manidipine | Calslot, Manyper | Cav1.x and Cav3.x blocker | Hypertension | Small Molecule | | |
Mavatrep | | TRPV1 antagonist | Pain | Small Molecule | | Janssen |
Memantine | Axura, Namenda | GluN antagonist | Moderate to severe Alzheimer's type dementia | Small molecule | 2003 | Forest labs |
Mepivacaine | Carbocaine | Nav inhibitor | Local anesthesia | Small molecule | 1960 FDA | Hospira, Inc., Pfizer |
Methoxyflurane | Penthrox | GABA-A activator, GluA1 inhibitor, GLYRA1 agonist | General anestesia | Small Molecule | | Abbott |
Methsuximide | Petinutin | Cav3.x blocker | Absence seizures, epilepsy | Small Molecule | 1957 | Parke Davis |
Mexiletine | Mexitil | Nav inhibitor | Ventricular arrhythmia | Small molecule | 1985 | |
Midazolam | Buccolam, Versed | GABA-A activator | Anxiety, Anesthesia, Status epilepticus | Small molecule | 1985 | |
Minoxidil | Loniten | Kir6.2 activator | Hypertension, alopecia | Small molecule | 1979 FDA | |
Mirogabalin | Tarlige | Cav ?2? modulator | Peripheral neuropathic pain | | | Daiichi Sankyo |
Nateglinide | Starlix | Kir6.2 blocker | Diabetes mellitus type 2 | Small molecule | 2000 FDA | Novartis |
Nicardipine | Cardene | Cav1.x inhibitor | Hypertension, angina pectoris | Small molecule | 1988 | |
Nicorandil | Ikorel, Dancor | Kir6.2 activator | Angina pectoris | Small molecule | 1984 | |
Nicotine | Nicorette, Nicotrol | Chrn agonist | Smoking cessation, nicotine dependence | Small molecule | | |
Nifedipine | Adalat, Procardia, Afeditab, Nifediac | Cav1.x blocker | Hypertension, vasospastic angina, premature labor | Small molecule | 1981 | Pfizer |
Nilvadipine | Escor, Escor forte, Naftdil, Nilvadipine, Nivadil, Towajil | calcium channel blocker | hypertension, vasospastic angina, chronic stable angina | Small Molecule | | Astellas Pharma, Archer Pharmaceuticals |
Nimodipine | Nimotop, Nymalize | Cav1.x blocker | Subarachnoid hemorrhage, hypertension | Small molecule | 1988 | |
Nisoldipine | Sular | Cav1.x blocker | Hypertension | Small Molecule | 1995 | Shionogi |
Nitrazepam | Mogadon, Alodorm, Nitrazadon | GABA-A potentiator | Insomnia | Small molecule | 1965 | |
Nitrendipine | Baypress, Nidrel | Cav1.x blocker | Hypertension | Small Molecule | 1985 | |
Ondansetron | Zophren | 5HT3A antagonist | Therapy-induced nausea and vomiting | Small molecule | 1991 FDA | GSK |
Oxazepam | Novoxapam, Alepam | GABA-A potentiator | Anxiety, alcohol withdrawal delirium | Small molecule | 1965 | |
Oxcarbazepine | Trileptal | Nav1.5 blocker | Epilepsy | Small molecule | 1990 | |
Oxybuprocaine | Novesine, Novesin | Nav inhibitor | Local anesthesia | Small Molecule | | |
Palonosetron | Aloxi | 5HT3A antagonist | Chemotherapy-induced nausea and vomiting | Small molecule | 2003 FDA 2009 EMA | Helsinn Healthcare |
Pentolinium | | NACHR antagonist | Hypertension | Small Molecule | | Wyeth Pharmaceuticals |
Perampanel | Fycompa | GluA1-4 antagonist | Partial seizures | Small molecule | 2012 FDA | Eisai |
Permethrin | Elimite | Sodium channel (Sarcoptes scabiei) inhibitor | Infestation by Sarcoptes scabiei, Pediculosis | Small Molecule | 1986 | |
Phenobarbital | Luminal | GABA-A potentiator | Epilepsy, Lennox-Gastaut syndrome, migraine | Small molecule | 1912 | |
Phensuximide | Milontin | Cav inhibitor Nav inhibitor | Epilepsy, absence seizures | Small molecule | FDA | Parke Davis |
Phenytoin | Dilantin | Nav inhibitor | Epilepsy | Small molecule | 1953 | Parke Davis |
Pinacidil | Pindac | Kir6.2 activator | Hypertension | Small molecule | 1989 FDA | Leo Pharma |
Pinaverium | Dicetel | Cav1.x antagonist | Irritable bowel syndrome | Small molecule | 1975 | Solvay Pharmaceuticals |
Pregabalin | Lyrica | Cav alpha-2/delta modulator | Diabetic peripheral neuropathy, postherpetic neuralgia | Small molecule | 2004 | |
Prilocaine | Citanest, Xylonest | Nav inhibitor | Local anaesthesia, premature ejaculation | Small molecule | 1965 | |
Primidone | Mysoline | GABA-A positive modulator | Epilepsy, Lennox-Gastaut syndrome | Small molecule | 1954 FDA | Valeant |
Procainamide | Pronestyl, Procan-SR, Procanbid | Nav inhibitor, Kv11.1 inhibitor | Life-threatening ventricular tachycardia | Small molecule | 1950 | Bristol-Meyers Squibb |
Procaine | Novocaine | Nav1.8 blocker | Local anesthesia | Small Molecule | 1954 | |
Propafenone | Rythmol | Nav1.5 blocker | Atrial fibrillation, atrial flutter, life-threatening ventricular tachycardia | Small molecule | 1989 | GSK |
Proparacaine | Alcaine, Ophthetic | Nav blocker | Local anesthesia | Small Molecule | 1953 | |
Propofol | Diprivan | GABA-A potentiator | General anaesthesia | Small molecule | 1989 FDA | Fresenius Kabi |
Quazepam | Doral, Dormalin | GABA-A potentiator | Insomnia | Small molecule | 1985 | Sciencure Pharma |
Quinidine | Cardioquin, Quinidex | Nav inhibitor | Atrial fibrillation, malaria, life-threatening ventricular tachycardia | Small Molecule | 1950 | Lilly |
Ranolazine | Ranexa | Nav inhibitor | Angina pectoris | Small molecule | 2006 | Gilead |
Repaglinide | Gluconorm, Prandin, Novonorm | Kir6.2 blocker | Diabetes mellitus type 2 | Small molecule | 1997 | Novo Nordisk |
Riluzole | Rilutek | KCa2.3 activator, Nav1.5 inhibitor | Amyotrophic lateral sclerosis | Small molecule | 1995 FDA | |
Rocuronium | Zemuron, Esmeron | Chrn a1b1d/g antagonist | General anaesthesia, muscle relaxation | Small molecule | 1994 FDA | |
Ropivacaine | Naropin | Nav blocker | Local anaesthesia | Small molecule | 1996 | Fresenius Kabi |
Rufinamide | Banzel | Nav modulator | Lennox-Gastaut syndrome | Small Molecule | 2007 EMA 2008 FDA | Novartis |
Safinamide | Xadago | Nav and Cav inhibitor | Parkinsons disease | Small Molecule | 2015 EMA 2017 FDA | Newron Pharmaceuticals |
Sevoflurane | Ultane, Sojourn | GABA-A activator, GLYRA1 agonist | General anestesia | Small Molecule | 1995 | Abbvie |
Sotalol | Biosotal, Sotalex | Kv11.1 blocker | Atrial fibrillation, life-threatening ventricular tachycardia | Small molecule | 1974 | |
Stiripentol | Diacomit | GABA-A positive modulator | Myoclonic seizures | Small Molecule | 2007 EMA 2018 FDA | Biocodex |
Succinylcholine | Anectine | Chrn a1b1deg agonist | General anaesthesia, muscle relaxation | Small molecule | 1952 FDA | Sandoz |
Temazepam | Restoril | GABA-A potentiator | Insomnia | Small molecule | 1981 | Mallinckrodt Pharmaceuticals |
Tetracaine | Pontocaine | Nav inhibitor | Local anesthesia | Small molecule | 1941 | |
Tezacaftor | | CFTR activator | Cystic fibrosis | Small Molecule | 2018 | Vertex Pharmaceuticals |
Tocainide | Tonocard | Nav blocker | Ventricular arrhythmia | Small Molecule | 1984 | |
Tolazamide | Tolinase, Norglycin | Kir6.2 inhibitor | Diabetes mellitus type 2 | Small molecule | 1966 | |
Tolbutamide | | Kir6.2 inhibitor | Diabetes mellitus type 2 | Small molecule | 1961 FDA | |
Topiramate | Topamax | GABA-A positive modulator, Nav blocker, GluA antagonist | Epilepsy, migraine, Lennox-Gastaut syndrome | Small Molecule | | |
Triamterene | Dyrenium | ENaC inhibitor | Hypertensive disorder, edema | Small molecule | 1964 | Smith Kline & French |
Triazolam | Halcion | GABA-A positive modulator | Insomnia | Small molecule | 1982 (withdrawn in the UK) | Pharmacia and Upjohn |
Trimebutine | Trimebutine | Cav1.x inhibitor, KCa inhibitor | Irritable bowel syndrome, postoperative paralytic ileus | Small Molecule | | |
Trimethadione | Tridione | Cav3.1 inhibitor | Absence seizures, epilepsy | Small Molecule | 1946 | Abbvie |
Unoprostone | Rescula | BK and CLC-2 activator | Ocular hypertension, open-angle glaucoma | Small Molecule | 2000 FDA (discontinued in the US) | Sucampo Pharmaceuticals |
Valproic acid | Convulex, Depakene, Valcote | Nav inhibitor, GABAA modulator | Epilepsy, absence seizures, bipolar disorder, migraine | Small molecule | | |
Varenicline | Chantix, Champix | Chrn a4b2 agonist | Smoking cessation | Small molecule | 2006 FDA | Pfizer |
Verapamil | Calan, Verelan | Cav1.x inhibitor | Hypertension, angina, supraventricular tachycardia, migraine, cluster headache | Small molecule | 1981 | |
Vernakalant | Brinavess | Nav1.5, Kv1.5, Kv4.3 blocker | Atrial fibrillation | Small Molecule | 2010, EMA | Cardiome Pharma |
XEP-018 | | NaV1.4 blocker | Skin wrinkles | Synthetic peptide | | Activen |
Zaleplon | Sonata | GABA-A agonist | Insomnia | Small Molecule | 1999 | Meda Ab, Pfizer |
Ziconotide | Prialt | Cav2.2 blocker | Severe and chronic pain | Synthetic peptide | 2004 | Elan Pharmaceuticals |
Zolpidem | Ambien | GABA-A agonist | Insomnia | Small molecule | 1992 | Sanofi Aventis |
Zonisamide | Zonegran | Nav blocker, Cav3.x blocker | Partial epilepsy | Small Molecule | 2000 | Eisai |
Zopiclone | Imovane, Zimovane | GABA-A potentiator | Insomnia | Small molecule | 1986 | Rhône-Poulenc |
Zucapsaicin | Zuacta | TRPV1 agonist | Severe pain associated with osteoarthritis of the knee, neuropathic pain | Small Molecule | | Sanofi Aventis |